6JPJ

Crystal structure of FGF401 in complex of FGFR4

6JPJ の概要

• エントリーDOI: 10.2210/pdb6jpj/pdb
• 分子名称: Fibroblast growth factor receptor 4, N-[5-cyano-4-(2-methoxyethylamino)pyridin-2-yl]-7-methanoyl-6-[(4-methyl-2-oxidanylidene-piperazin-1-yl)methyl]-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide, SULFATE ION, ... (4 entities in total)
• 機能のキーワード: fgf401, reversible covalent inhibitor, fgfr4, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 35361.67

構造登録者

Zhou, Z.,Chen, X.,Chen, Y. (登録日: 2019-03-27, 公開日: 2019-05-15, 最終更新日: 2024-10-16)

主引用文献

Zhou, Z.,Chen, X.,Fu, Y.,Zhang, Y.,Dai, S.,Li, J.,Chen, L.,Xu, G.,Chen, Z.,Chen, Y.
Characterization of FGF401 as a reversible covalent inhibitor of fibroblast growth factor receptor 4.
Chem.Commun.(Camb.), 55:5890-5893, 2019

PubMed Abstract: Biochemical and structural studies provide information on the mode of action of FGF401 as a selective, reversible covalent inhibitor of FGFR4. Kinase and proliferation assays reveal that FGF401 has the ability to overcome gatekeeper mutations in FGFR4.

PubMed: 31041948
DOI: 10.1039/c9cc02052g

実験手法

X-RAY DIFFRACTION (2.638 Å)